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| 品牌 | absin | CAS | 863031-21-4 |
|---|---|---|---|
| 分子式 | C30H24N4O8 | 纯度 | 98% |
| 分子量 | 568.53 | 货号 | abs47028281 |
| 规格 | 2mg | 供货周期 | 现货 |
| 主要用途 | is a potent angiotensin II type 1 (AT1) | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Azilsartan Medoxomil 863031-21-4
| 产品描述 | |
| 描述 | Azilsartan Medoxomil is a potent angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS, with an IC50 of 2.6 nM, exhibits >10,000-fold selectivity over AT2. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 阿奇沙坦酯 |
| 可溶性/溶解性 | DMSO :114 mg/mL (200.51 mM) |
| 生物活性 | |
| 靶点 | AT1 receptor |
| In vitro(体外研究) | Azilsartan medoxomil is a prodrug, which is rapidly converted to the active moiety, azilsartan (TAK-536), by ester hydrolysis in the gut and plasma during absorption after oral administration. Azilsartan selectively blocks the binding of angiotensin II to the AT1 (angiotensin II type 1) receptors found in the vascular smooth muscle and the adrenal gland, thereby promoting vasodilation and a decrease in the effects of aldosterone. Azilsartan is a highly selective antagonist to the AT1 receptor, with an IC50 of 2.6 nM, exhibiting a >10,000-fold affinity for the AT1 receptor compared with the AT2 receptor, and has not shown affinity for other cardiac receptors or ion channels. The inhibitory effect of Azilsartan persists after washout of the free compound (IC50 value of 7.4 nM). Azilsartan also inhibits the accumulation of angiotensin II -induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM, and this effect is resistant to washout (IC50 value of 81.3 nM). |
| 参考文献 | |
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| 研究领域 | |
| 研究领域 | Cardiovascular NeuroscienceEndocrine system Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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